F. Dolle et al., Highly efficient synthesis of [C-11]PE2I, a selective radioligand for the quantification of the dopamine transporter using PET, J LABEL C R, 43(10), 2000, pp. 997-1004
PE2I ((E)-N-(3-iodoprop-2-enyl)-2 beta-carbomethoxy-3 beta-(4'-tolyl) nortr
opane) is a cocaine derivative belonging to a new generation of selective d
opamine transporter inhibitors. Labelled with iodine-123 (half-life : 13.1
hours), PE2I has been dedicated to the diagnostics of neurodegenerative dis
eases such as Parkinson's disease in humans using single photon emission co
mputed tomography. Labelled with carbon-11 (half-life : 20.4 minutes), it c
an be used in the absolute quantification of the dopamine transporter (DAT)
using the high-resolution, sensitive and non-invasive quantitative imaging
technique PET (positron emission tomography). In this paper, the radiosynt
hesis of carbon-ii labelled PE2I was investigated and oriented towards the
preparation of multi milliCuries of radiotracer. Typically, 200 to 300 mCi
(7.4-11.1 GBq) of [C-11]PE2I were routinely obtained within 25 minutes of r
adiosynthesis (including HPLC purification) with specific radioactivities r
anging from 0.8 to 1.2 Ci/mu mol (29.6-44.4 GBq/mu mol). Based on the preli
minary PET experiments, it can be assumed that this radioligand would permi
t quantification of the DAT using PET and mathematical compartmental ligand
-transporter models.